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Pomaglumetad methionil

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Pomaglumetad methionil
Clinical data
Other namesLY-2140023; LY2140023; LY-2812223; LY2812223; Pomaglumetad prodrug; LY-404039 prodrug; DB-103; DB103
Routes of
administration		Oral[1][2]
Drug classMetabotropic glutamate mGlu2 and mGlu3 receptor agonist
ATC code
  • None
Pharmacokinetic data
Bioavailability49%[2]
Protein bindingMinimal[2]
Elimination half-life1.5–2.4 hours[2]
Pomaglumetad: 2–6.2 hours[2]
Identifiers
  • (1R,4S,5S,6S)-4-[[(2S)-2-amino-4-methylsulfanylbutanoyl]amino]-2,2-dioxo-2λ6-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC12H18N2O7S2
Molar mass366.40 g·mol−1
3D model (JSmol)
  • CSCC[C@@H](C(=O)N[C@]1(CS(=O)(=O)[C@@H]2[C@H]1[C@H]2C(=O)O)C(=O)O)N
  • InChI=1S/C12H18N2O7S2/c1-22-3-2-5(13)9(15)14-12(11(18)19)4-23(20,21)8-6(7(8)12)10(16)17/h5-8H,2-4,13H2,1H3,(H,14,15)(H,16,17)(H,18,19)/t5-,6+,7+,8-,12-/m0/s1
  • Key:VOYCNOJFAJAILW-CAMHOICYSA-N

Pomaglumetad methionil (INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name; developmental code names LY-2140023 and LY-2812223) is a metabotropic glutamate mGlu2 and mGlu3 receptor agonist which is or was under development for the treatment of schizophrenia, substance-related disorders, and post-traumatic stress disorder (PTSD).[1][2] It is taken orally.[1][2]

Pharmacology

[edit]

The drug is an inactive prodrug of pomaglumetad (LY-404039), which acts as a highly selective metabotropic glutamate mGlu2 and mGlu3 receptor agonist.[2] Whereas the oral bioavailability of pomaglumetad was found to be low in humans, pomaglumetad methionil has an estimated oral bioavailability of approximately 49%.[2] The drug is transported by the peptide transporter 1 (PepT1), resulting in it being rapidly and efficiently absorbed, and is then hydrolyzed into pomaglumetad.[2] The elimination half-life of pomaglumetad methionil is 1.5 to 2.4 hours, whereas the half-life of pomaglumetad is 2 to 6.2 hours.[2]

Development

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Pomaglumetad methionil was under development by Eli Lilly and Company, Denovo Biopharma, and other institutions.[1][3] As of January 2025, no recent development has been reported for treatment of schizophrenia or substance-related disorders, whereas development has been discontinued for PTSD.[1][3] The highest developmental stage that pomaglumetad methionil has reached is phase 2 clinical trials.[1][3]

See also

[edit]

References

[edit]
  1. ^ a b c d e f "Pomaglumetad methionil - Denovo Biopharma/Eli Lilly and Company". AdisInsight. 28 January 2025. Retrieved 1 October 2025.
  2. ^ a b c d e f g h i j k Kinon BJ, Gómez JC (March 2013). "Clinical development of pomaglumetad methionil: a non-dopaminergic treatment for schizophrenia". Neuropharmacology. 66: 82–86. doi:10.1016/j.neuropharm.2012.06.002. PMID 22722029.
  3. ^ a b c "Delving into the Latest Updates on Pomaglumetad methionil with Synapse". Synapse. 23 September 2025. Retrieved 1 October 2025.



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